- Oxidative kinetic resolution of heterocyclic sulfoxides with a porphyrin-inspired manganese complex by hydrogen peroxide
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We have successfully reported here the low loading porphyrin-inspired high-valent manganese (IV)-oxo complex was applied in oxidative kinetic resolution (OKR) of racemic heterocyclic sulfoxides using the environmentally benign hydrogen peroxide for the first time. This approach allows for rapid OKR (0.5 h) of a variety of racemic sulfoxides (including pyridine, pyrimidine, pyrazine, thiazole, benzothiazole, thiophene) in excellent enantioselectivity (up to > 99% ee), simultaneously generating the corresponding sulfones in high yield (up to 80%). The catalytic system also showed an unexceptionable chemoselectivity for the sulfoxide substrates with hydroxyl groups in which only the sulfoxide group was oxidized. The practical utility of the method has been demonstrated in the OKR of gram-scale sulfoxides.
- Yang, Jinchuang,Wang, Lianyue,Lv, Ying,Li, Ning,An, Yue,Gao, Shuang
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supporting information
p. 156 - 159
(2017/12/15)
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- GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
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A compound, enantiomer, prodrug, diastereomer, or salt is provided which is an activator of the enzyme glucokinase and thus is believed to be useful in treating diabetes and related diseases, which compound has the structure (I). A method for treating diabetes and related disease employing the compound, enantiomer, prodrug, diastereomer, or salt is also provided.
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- TRICYCLIC COMPOUND FOR BROMODOMAIN-CONTAINING PROTEIN INHIBITOR AND PREPARATION, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
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The present applicationpresent application relates to a compound represented by Formula (III) or a pharmaceutically acceptable salt, solvent compound, active metabolite, crystal polymorph, ester, isomer, or prodrug thereof. The application further provides a pharmaceutical composition comprising the compound represented by Formula (III) and a use thereof for preparing a bromodomain inhibitor for preventing or treating various diseases, such as inflammation and cancer, related to the bromodomain.
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- NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, W and X are as described herein, compositions including the compounds and methods of using the compounds.
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- Pyridonaphthyridine PI3K/MTOR Dual Inhibitors and Preparation and Use Thereof
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The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
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- PYRIDONAPHTHYRIDINE PI3K/MTOR DUAL INHIBITORS AND PREPARATION AND USE THEREOF
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The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
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- BICYCLIC COMPOUNDS AND USE AS ANTIDIABETICS
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The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.
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Page/Page column 40
(2010/03/02)
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- 1, 3 - DIHYDROXY SUBSTITUTED PHENYLAMIDE GLUCOKINASE ACTIVATORS
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Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is alkyl, aryl, arylalkyl, heteroaryl, or he
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Page/Page column 108-109
(2009/01/24)
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- SUBSTITUTED ARYLCYCLOPROPYLACETAMIDES AS GLUCOKINASE ACTIVATORS
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According to the present invention there is provided a compounds of formula (I): and pharmaceutically acceptable salts thereof.
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Page 104-105
(2008/06/13)
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- Selective monolithiation of 2,5-dibromopyridine with butyllithium
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Selective monolithiation of 2,5-dibromopyridine at either the 2-position or the 5-position is reported. Solvent and concentration strongly influence the selectivity. Coordinating solvents and higher concentration favor the 5- position while non-coordinati
- Wang, Xin,Rabbat, Philippe,O'Shea, Paul,Tillyer, Richard,Grabowski,Reider, Paul J.
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p. 4335 - 4338
(2007/10/03)
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- THE REACTIONS OF SOME HALOGENATED PYRIDINES WITH METHOXYDE AND METHANETHIOLATE IONS IN DIMETHYLFORMAMIDE
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The reactions of 2,6- and 2,5-dibromopyridines and of 2,3- and 3,5-dichloropyridines with sodium isopropanethiolate and methanethiolate afforded the products of mono- or of bis-substitution depending on the experimental conditions.The same pyridines reacted with sodium methoxide to give good yields of the mono-substituted products; bis-substitution occurred easily only in the case of the 2,6-dibromo- and of the 3,5-dichloropyridine.The syntheses of some methoxy thiomethoxypyridine, starting from the halogeno methoxypyridines or from the halogeno thiomethoxypyridines are also described.The bis-(alkylthio)pyridines can be fragmented by sodium in HMPA to give the bis(mercapto)pyridines.
- Testaferri, Lorenzo,Tiecco, Marcello,Tingoli, Marco,Bartoli, Donatella,Massoli, Alberto
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p. 1373 - 1384
(2007/10/02)
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